反应详情

温度

75 °C

To a solution of N-(4-fluoro-2-methylphenyl)azetidin-3-amine (D55) and triethylamine (0.14 ml, 1.04 mmol) in tetrahydrofuran/methanol (3 ml/1 ml) methyl 4-(1-(2,5-dichloronicotinamido)cyclopropyl)benzoate (D97) (253 mg, 0.693 mmol) was added and the resulting mixture was heated 24 h at 75° C. The residue obtained after solvent evaporation, was purified by Biotage SNAP-Si (10 g) cartridge eluting with eluting with a mixture dichloromethane/ethylacetate from 95/5 to 80/20. Collected fractions, after solvent evaporation afforded the title compound (D168) (105 mg).

1. customThe residue obtained
2. customafter solvent evaporation
3. customwas purified by Biotage SNAP-Si (10 g) cartridge
4. washeluting
5. washwith eluting with a mixture dichloromethane/ethylacetate from 95/5 to 80/20
6. customCollected fractions, after solvent evaporation